| 摘要 |
<p>NEW MATERIAL:5-Halogenouracil derivatives of formula VI and VIII(R<2> is alkyl, alkyl, cycloalkyl, aralkyl, aryl; Y is Cl, Br, I. EXAMPLE:1-(5-Chloro-1H-2-oxopyrimidine-4-yl)-beta-D-glucopyranouronic acid. USE:Carcinostatic and antiviral agents. They are O<4>-glucuronide derivatives of 5-halogenouracil and low toxic. PREPARATION:A metal salt of 5-halogenouracil of formula II (R<3> is benzyl or hydroyl group-protecting group that can be eliminated by reduction; M is silver, HgCl) and a halogenoglucopyranouronic ester derivative of formula III (R<4> is acyl) are subjected to condensation reaction to form a compound of formula IV, from which protecting groups are eliminated to prepare the objective compound of formula VI and VIII.</p> |
